Preparation method of VEGFR inhibitor tevozanib

A technology of tivozanib and mixed solvent, which is applied in the field of preparation of VEGFR inhibitor tivozanib, can solve problems such as the need for improvement of tivozanib, avoid the occurrence of side reactions, improve reaction safety, and reduce reaction temperature Effect

Pending Publication Date: 2022-03-22
武汉九州钰民医药科技有限公司
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Problems solved by technology

[0006] Yet, the preparation method of Tivo

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  • Preparation method of VEGFR inhibitor tevozanib
  • Preparation method of VEGFR inhibitor tevozanib
  • Preparation method of VEGFR inhibitor tevozanib

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Embodiment Construction

[0039] Embodiments of the present invention are described in detail below. The embodiments described below are exemplary only for explaining the present invention and should not be construed as limiting the present invention. If no specific technique or condition is indicated in the examples, it shall be carried out according to the technique or condition described in the literature in this field or according to the product specification. The reagents or instruments used were not indicated by the manufacturer, and they were all commercially available conventional products.

[0040] Synthesis of compound shown in embodiment 1 formula 3

[0041] Under a nitrogen atmosphere at about -78 ° C, the compound shown in Formula 1 (14.36 g, 0.1 mol) and the compound shown in Formula 2 (22.0 g, 0.11 mol) were added to CH 2 Cl 2 (300mL), then slowly add Tf 2 O (33.86g, 0.12mol), the resulting mixture was maintained at about -78°C and stirred for 15min, then warmed up to room temperatur...

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Abstract

The invention relates to a preparation method of a VEGFR (vascular endothelial growth factor receptor) inhibitor tevozanib. Compared with the prior art, according to the preparation method, the compound shown in the formula 1 and the compound shown in the formula 2 are selected to react, the reaction reagent compound shown in the formula 3 is prepared firstly, then the reaction reagent compound shown in the formula 3 and the hydroxyl of the compound shown in the formula 4 are subjected to the substitution reaction, the reaction site of the reaction is single, the yield is excellent, and reaction purification is convenient; the method provided by the invention has the advantages of simple operation process, low purification cost and high overall yield, and is suitable for industrial large-scale production of bulk pharmaceutical chemicals, and the process steps for synthesizing and preparing the tevozanib are simplified.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to a preparation method of a VEGFR inhibitor tivozanib. Background technique [0002] Tivozanib (trade name Fotivda) is a tyrosine kinase inhibitor. In vitro cellular kinase assays demonstrated that tivozanib inhibited the phosphorylation of vascular endothelial growth factor receptor (VEGFR)-1, VEGFR-2, and VEGFR-3 at clinically relevant concentrations and inhibited other kinases, including c-kit and PDGFRβ, as well as tumor growth in various tumor cell types, including human renal cell carcinoma. [0003] Tivozani was originally discovered by Kyowa Hakko Kirin in Japan, and was first approved in the European Union for the treatment of advanced renal cell carcinoma (RCC) in August 2017. On March 10, 2021, the U.S. FDA approved AVEO PHARMS' tivozanib capsules for the treatment of adults with relapsed or refractory advanced renal cell carcinoma after two or more prior systemic ...

Claims

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Application Information

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IPC IPC(8): C07D413/12
CPCC07D413/12
Inventor 陈程黄祥泉范昭泽
Owner 武汉九州钰民医药科技有限公司
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